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Literature summary for 3.1.1.1 extracted from
- Inhibition of carboxylesterase activity of THP1 monocytes/macrophages and recombinant human carboxylesterase 1 by oxysterols and fatty acids (2010), Biochim. Biophys. Acta, 1801, 31-41.
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| (10Z)-hexadecenoic acid | - |
Homo sapiens |  |
| (5Z,8Z,11Z,14Z)-eicosatetraenoic acid | - |
Homo sapiens | |
| (6Z,9Z,12Z)-octadecatrienoic acid | - |
Homo sapiens | |
| (9Z)-octadecenoic acid | - |
Homo sapiens | |
| (9Z)-tetradecenoic acid | - |
Homo sapiens | |
| (9Z,12Z)-octadecadienoic acid | - |
Homo sapiens | |
| 11,12-epoxy-(5Z,8Z,14Z)-eicosatrienoic acid | - |
Homo sapiens | |
| 14,15-epoxy-(5Z,8Z,11Z)-eicosatrienoic acid | - |
Homo sapiens | |
| 15-deoxy-DELTA12,14-prostaglandin J2 | - |
Homo sapiens | |
| 22(R)-hydroxycholesterol | slight inhibition of CES1, not CES2 | Homo sapiens | |
| 24(S),25-epoxycholesterol | inhibits only CES1, not CES2 | Homo sapiens | |
| 24(S)-hydroxycholesterol | slight inhibition of CES1, not CES2 | Homo sapiens | |
| 25-hydroxycholesterol | slight inhibition of CES1, not CES2 | Homo sapiens | |
| 27-Hydroxycholesterol | partially noncompetitive inhibitor of recombinant CES1, impaires intracellular CES1 activity following treatment of intact THP1 cells. No inhibition of CES2 | Homo sapiens | |
| 7-oxocholesterol | slight inhibition of CES1, not CES2 | Homo sapiens | |
| arachidonic acid | most potent fatty acid inhibitor of recombinant CES1 acting by a noncompetitive mechanism, overview. The inhibition is reversible by bovine serum albumin | Homo sapiens | |
| benzil | inhibition of CES1 in THP-1 cells | Homo sapiens | |
| bioresmethrin | a pyrethroid insecticide | Homo sapiens | |
| cholesterol | slight inhibition of CES1, not CES2 | Homo sapiens | |
| hexadecanoic acid | - |
Homo sapiens | |
| additional information | unsaturated fatty acids are better inhibitors of CES1 activity than saturated fatty acids, CES2 activity is unaffected by any fatty acid | Homo sapiens | |
| octadecanoic acid | - |
Homo sapiens | |
| paraoxon | inhibition of CES1 in THP-1 cells | Homo sapiens | |
| prostaglandin E2 | - |
Homo sapiens | |
| prostaglandin F2alpha | - |
Homo sapiens | |
| tetradecanoic acid | - |
Homo sapiens | |
| trans-permethrin | a pyrethroid insecticide | Homo sapiens | |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| additional information | Homo sapiens | xenobiotic substrates are pyrethroid insecticides | ? | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
isozymes CES1 and CES2 | - |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| liver | CES1 and CES2, S9 fraction, HL1220 and HL1274 | Homo sapiens | - |
| macrophage | CES1, no expression of CES2 | Homo sapiens | - |
| monocyte | CES1, no expression of CES2 | Homo sapiens | - |
| THP-1 cell | CES1, no expression of CES2 | Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| 4-nitrophenyl valerate + H2O | - |
Homo sapiens | 4-nitrophenol + valerate | - |
? | |
| additional information | xenobiotic substrates are pyrethroid insecticides | Homo sapiens | ? | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| carboxylesterase 1 | - |
Homo sapiens |
| CES1 | - |
Homo sapiens |
| CES2 | - |
Homo sapiens |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 37 | - |
assay at | Homo sapiens |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 7.4 | - |
assay at | Homo sapiens |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| additional information | - |
additional information | inhibition kinetics | Homo sapiens | |
| 0.00001 | - |
27-Hydroxycholesterol | pH 7.4, 37°C, recombinant CES1 | Homo sapiens | |
| 0.0018 | - |
arachidonic acid | pH 7.4, 37°C, recombinant CES1 | Homo sapiens | |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.000033 | - |
pH 7.4, 37°C, recombinant CES1 | Homo sapiens | 27-Hydroxycholesterol | |
| 0.002 | - |
pH 7.4, 37°C, recombinant CES1 | Homo sapiens | (5Z,8Z,11Z,14Z)-eicosatetraenoic acid | |
| 0.007 | - |
pH 7.4, 37°C, recombinant CES1 | Homo sapiens | (9Z)-octadecenoic acid | |
| 0.007 | - |
pH 7.4, 37°C, recombinant CES1 | Homo sapiens | (10Z)-hexadecenoic acid | |
| 0.0081 | - |
pH 7.4, 37°C, recombinant CES1 | Homo sapiens | 24(S),25-epoxycholesterol | |
| 0.009 | - |
pH 7.4, 37°C, recombinant CES1 | Homo sapiens | tetradecanoic acid | |
| 0.009 | - |
pH 7.4, 37°C, recombinant CES1 | Homo sapiens | (9Z,12Z)-octadecadienoic acid | |
| 0.012 | - |
pH 7.4, 37°C, recombinant CES1 | Homo sapiens | (9Z)-tetradecenoic acid | |
| 0.013 | - |
pH 7.4, 37°C, recombinant CES1 | Homo sapiens | 15-deoxy-DELTA12,14-prostaglandin J2 | |
| 0.019 | - |
pH 7.4, 37°C, recombinant CES1 | Homo sapiens | (6Z,9Z,12Z)-octadecatrienoic acid | |
| 0.025 | - |
pH 7.4, 37°C, recombinant CES1 | Homo sapiens | hexadecanoic acid | |
| 0.027 | - |
pH 7.4, 37°C, recombinant CES1 | Homo sapiens | 11,12-epoxy-(5Z,8Z,14Z)-eicosatrienoic acid | |
| 0.038 | - |
pH 7.4, 37°C, recombinant CES1 | Homo sapiens | 14,15-epoxy-(5Z,8Z,11Z)-eicosatrienoic acid | |
| 0.1 | - |
pH 7.4, 37°C, recombinant CES1 | Homo sapiens | prostaglandin E2 | |
| 0.1 | - |
pH 7.4, 37°C, recombinant CES1 | Homo sapiens | prostaglandin F2alpha | |
| 0.1 | - |
pH 7.4, 37°C, recombinant CES1 | Homo sapiens | octadecanoic acid | |
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